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2-[3-[3-[[2-氯-3-(三氟甲基)芐基](2,2-二苯基乙基)氨基]丙氧基]苯基]乙酸鹽酸鹽
化合物 GW3965 HCl
化合物 GW3965 HCl|T6310|TargetMol
價(jià)格
¥
228
¥
329
¥
578
包裝
1mg
2mg
5mg
最小起訂量
1mg
發(fā)貨地
上海
更新日期
2024-12-12
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產(chǎn)品詳情
中文名稱:
化合物 GW3965 HCl
英文名稱:
GW3965 hydrochloride
CAS:
405911-17-3
品牌:
TargetMol
產(chǎn)地:
美國
保存條件:
store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
純度規(guī)格:
99.51%
產(chǎn)品類別:
抑制劑
貨號(hào):
T6310
2024-12-12
化合物 GW3965 HCl
GW3965 hydrochloride
1mg/228RMB;2mg/329RMB;5mg/578RMB
228
TargetMol
美國
store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
99.51%
抑制劑
Product Introduction
Bioactivity
名稱
GW3965 hydrochloride
描述
GW3965 hydrochloride (GW3965 HCl) is an effective and specific LXR agonist for hLXRα/β (EC50: 190/30 nM).
細(xì)胞實(shí)驗(yàn)
Cells are seeded in 96 wells and are treated after 24 hours with different drugs indicated in each experiment in medium containing 1% FBS or lipoprotein deficient serum. Relative proliferation is determined using Cell Proliferation Assay Kit. Cells are incubated 1.5 hrs after adding tetrazolium salt WST-1 [2-(4-iodophenyl)-3- (4-nitrophenyl)-5-(2, 4-disulfo-phenyl)-2H-tetrazolium, monosodium salt] at 5% CO2, 37oC and the absorbance of the treated and untreated cells are measured using a microplate reader at 420 to 480 nm. Cells seeded in 12 well plates are counted using a hemocytometer, and dead cells are assessed using trypan blue exclusion assays.
激酶實(shí)驗(yàn)
Steady-state drug accumulation assay: AuxB1 and CHrB30 cells are grown to confluency in 12-well (24 mm) tissue culture dishes and the steady-state accumulation of [3H]-vinblastine is measured. Accumulation is initiated by the addition of 0.1 μ Ci [3H]-vinblastine and unlabelled vinblastine to a final concentration of 100 nM . The accumulation of [3H]-paclitaxel is measured using 0.1 μ Ci [3H]-paclitaxel and unlabelled drug to a final concentration of 1 μM . Cells are incubated in a reaction volume of 1 mL for 60 min at 37 ℃ under 5% CO2 in order to reach steady-state. The effect of the modulators XR9576 on [3H]-ligand accumulation is investigated in the concentration range 10-9 - 10-6 M. Modulators are added from a DMSO stock giving a final solvent concentration of 0.2 % (v/v). Following cell harvesting, accumulated drug is measured by liquid scintillation counting and normalized for cell protein content. Plots of amount accumulated as a function of modulator concentration are fitted with the general dose-response equation: Y={(a-b)/(1+(X/c)d)}+b Where: Y=response; a=initial response; b=final response; c=EC50 concentration; d=slope value; X=drug concentration.
體外活性
GW3965 recruits the steroid receptor coactivator 1 to human LXRα with EC50 of 125 nM in a cell-free ligand-sensing assay. [1] GW3965 shows a potent antagonistic activity against hLXRα and hLXRβ in cell-based assays with EC50 of 190 nM and 30 nM, respectively. Besides, GW3965 also sows excellent selectivity over other nuclear receptors. [1] In human islets, GW3965 (1 μM) reduces expression of selected pro-inflammatory cytokines including IL-8, monocyte chemotactic protein-1 and tissue factor. [4]
體內(nèi)活性
In mice, GW3965 at a dose of 10 mg/kg upregulates ABCA1 expression 8-fold and raises circulating levels of HDL by 30% with Cmax of 12.7 μg/mL and t1/2 of 2 hours. [1] GW3965 (10 mg/kg) induces expression of ABCA1 and ABCG1 and shows potent antiatherogenic activity in both LDLR?/? and apoE?/? mice. [2] In male sprague-dawley rats, GW3965 reduces Ang II-mediated increases in blood pressure and decreases vascular Ang II receptor gene expression. [3] In Glioblastoma mouse model, GW3965 results in inducible degrader of LDLR-mediated LDLR degradation, increased expression of the ABCA1 cholesterol efflux transporter, and thus potently promotes tumor cell death. [5]
存儲(chǔ)條件
store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度
DMSO : 61.9 mg/mL (100 mM)
Ethanol : 12.4 mg/mL (20 mM)
關(guān)鍵字
GW-3965 | Liver X receptor | GW-3965 hydrochloride | Inhibitor | GW3965 | inhibit | GW3965 Hydrochloride | LXR | GW-3965 Hydrochloride | GW3965 hydrochloride | GW 3965 | GW 3965 Hydrochloride
相關(guān)產(chǎn)品
SR9243 | (20S)-Protopanaxatriol | RGX-104 hydrochloride | 27-Hydroxycholesterol | T0901317 | GW6340 | Rovazolac | GSK2033 | SR9238 | RGX-104 | BE1218 | GAC0003A4
相關(guān)庫
脂代謝化合物庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 代謝化合物庫 | 含氟化合物庫 | 抗心血管疾病化合物庫 | NO PAINS 化合物庫 | 臨床前化合物庫 | 核受體化合物庫 | 抗代謝疾病化合物庫
關(guān)鍵字:
GW3965 HCl|TargetMol
公司簡介
TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓,致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國家和地區(qū),已發(fā)展成為全球知名的化合物庫和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫,以及多種類型的生化試劑產(chǎn)品,包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等,此外,我們還建設(shè)有CADD(計(jì)算機(jī)輔助藥物設(shè)計(jì))研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心,全方位滿足客戶的定制需求。 憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持,我們將有效幫助您縮短研發(fā)周期,取得更成功的結(jié)果。
成立日期
2013-04-18
(12年)
注冊(cè)資本
566.265100萬人民幣
員工人數(shù)
100-500人
年?duì)I業(yè)額
¥ 1億以上
主營行業(yè)
天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù)
經(jīng)營模式
貿(mào)易,工廠,試劑,定制,服務(wù)
TargetMol中國(陶術(shù)生物)
VIP
3年
公司成立:
12年
注冊(cè)資本:
566.265100萬人民幣
企業(yè)類型:
有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品:
小分子抑制劑、藥物篩選化合物庫、藥物篩選等
公司地址:
靜安區(qū)江場三路238號(hào)8樓
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產(chǎn)品名稱
價(jià)格
公司名稱
報(bào)價(jià)日期
aladdin 阿拉丁 G408657 GW3965 HCl 405911-17-3 10mM in DMSO
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1年
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aladdin 阿拉丁 G129708 GW3965 鹽酸鹽 405911-17-3 ≥97%
¥926.90
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